Toremifene

DB00539

small molecule approved investigational

Deskripsi

Toremifene is a selective estrogen receptor modulator (SERM) and a nonsteroidal antiestrogen used to treat estrogen receptor positive breast cancer.A256923 Like tamoxifen, toremifene is part of the first-generation triphenylethylene derivative chemical class of SERMs.A256928

Toremifene possesses tissue-specific actions: it has estrogenic (agonist) activity on the cardiovascular system and on bone tissue and it has weak estrogenic effects on uterine tissue, however, it also has antiestrogenic (estrogen-antagonist) activity on breast tissue.A256923

Struktur Molekul 2D

Berat 405.96
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 5 days
Volume Distribusi * 580 L
Klirens (Clearance) * 5 L/h

Absorpsi

Well absorbed

Metabolisme

Hepatic. Mainly by CYP3A4 to N-demethyltoremifene, which exhibits antiestrogenic effects but has weak antitumor potency in vivo.

Rute Eliminasi

Toremifene is extensively metabolized, principally by CYP3A4 to N-demethyltoremifene, which is also antiestrogenic but with weak in vivo antitumor potency.

Interaksi Makanan

2 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits CYP3A4 and therefore, may elevate toremifene serum levels.
  • 2. Take with or without food.

Interaksi Obat

724 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Toremifene.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Toremifene.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Toremifene.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Toremifene.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Toremifene.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Toremifene.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Toremifene.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Toremifene.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Toremifene.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Toremifene.
Silodosin The excretion of Silodosin can be decreased when combined with Toremifene.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Toremifene.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Toremifene.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Toremifene.
Methyclothiazide The risk or severity of hypercalcemia can be increased when Methyclothiazide is combined with Toremifene.
Chlorthalidone The risk or severity of hypercalcemia can be increased when Chlorthalidone is combined with Toremifene.
Bendroflumethiazide The risk or severity of hypercalcemia can be increased when Bendroflumethiazide is combined with Toremifene.
Metolazone The risk or severity of hypercalcemia can be increased when Metolazone is combined with Toremifene.
Benzthiazide The risk or severity of hypercalcemia can be increased when Benzthiazide is combined with Toremifene.
Hydroflumethiazide The risk or severity of hypercalcemia can be increased when Hydroflumethiazide is combined with Toremifene.
Indapamide The risk or severity of hypercalcemia can be increased when Indapamide is combined with Toremifene.
Chlorothiazide The risk or severity of hypercalcemia can be increased when Chlorothiazide is combined with Toremifene.
Hydrochlorothiazide The risk or severity of hypercalcemia can be increased when Hydrochlorothiazide is combined with Toremifene.
Trichlormethiazide The risk or severity of hypercalcemia can be increased when Trichlormethiazide is combined with Toremifene.
Polythiazide The risk or severity of hypercalcemia can be increased when Polythiazide is combined with Toremifene.
Quinethazone The risk or severity of hypercalcemia can be increased when Quinethazone is combined with Toremifene.
Cyclopenthiazide The risk or severity of hypercalcemia can be increased when Cyclopenthiazide is combined with Toremifene.
Epitizide The risk or severity of hypercalcemia can be increased when Epitizide is combined with Toremifene.
Ospemifene The risk or severity of adverse effects can be increased when Toremifene is combined with Ospemifene.
Sugammadex The therapeutic efficacy of Sugammadex can be decreased when used in combination with Toremifene.
Lepirudin The risk or severity of bleeding can be increased when Toremifene is combined with Lepirudin.
Bivalirudin The risk or severity of bleeding can be increased when Toremifene is combined with Bivalirudin.
Alteplase The risk or severity of bleeding can be increased when Toremifene is combined with Alteplase.
Urokinase The risk or severity of bleeding can be increased when Toremifene is combined with Urokinase.
Reteplase The risk or severity of bleeding can be increased when Toremifene is combined with Reteplase.
Anistreplase The risk or severity of bleeding can be increased when Toremifene is combined with Anistreplase.
Tenecteplase The risk or severity of bleeding can be increased when Toremifene is combined with Tenecteplase.
Abciximab The risk or severity of bleeding can be increased when Toremifene is combined with Abciximab.
Drotrecogin alfa The risk or severity of bleeding can be increased when Toremifene is combined with Drotrecogin alfa.
Streptokinase The risk or severity of bleeding can be increased when Toremifene is combined with Streptokinase.
Dicoumarol The risk or severity of bleeding can be increased when Toremifene is combined with Dicoumarol.
Argatroban The risk or severity of bleeding can be increased when Toremifene is combined with Argatroban.
Ardeparin The risk or severity of bleeding can be increased when Toremifene is combined with Ardeparin.
Phenindione The risk or severity of bleeding can be increased when Toremifene is combined with Phenindione.
Fondaparinux The risk or severity of bleeding can be increased when Toremifene is combined with Fondaparinux.
Warfarin The risk or severity of bleeding can be increased when Toremifene is combined with Warfarin.
Pentosan polysulfate The risk or severity of bleeding can be increased when Toremifene is combined with Pentosan polysulfate.
Phenprocoumon The risk or severity of bleeding can be increased when Toremifene is combined with Phenprocoumon.
Dipyridamole The risk or severity of bleeding can be increased when Toremifene is combined with Dipyridamole.
Heparin The risk or severity of bleeding can be increased when Toremifene is combined with Heparin.
Enoxaparin The risk or severity of bleeding can be increased when Toremifene is combined with Enoxaparin.
Epoprostenol The risk or severity of bleeding can be increased when Toremifene is combined with Epoprostenol.
Acenocoumarol The risk or severity of bleeding can be increased when Toremifene is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of bleeding can be increased when Toremifene is combined with 4-hydroxycoumarin.
Coumarin The risk or severity of bleeding can be increased when Toremifene is combined with Coumarin.
Ximelagatran The risk or severity of bleeding can be increased when Toremifene is combined with Ximelagatran.
Desmoteplase The risk or severity of bleeding can be increased when Toremifene is combined with Desmoteplase.
Defibrotide The risk or severity of bleeding can be increased when Toremifene is combined with Defibrotide.
Ancrod The risk or severity of bleeding can be increased when Toremifene is combined with Ancrod.
Beraprost The risk or severity of bleeding can be increased when Toremifene is combined with Beraprost.
Prasugrel The risk or severity of bleeding can be increased when Toremifene is combined with Prasugrel.
Rivaroxaban The risk or severity of bleeding can be increased when Toremifene is combined with Rivaroxaban.
Sulodexide The risk or severity of bleeding can be increased when Toremifene is combined with Sulodexide.
Semuloparin The risk or severity of bleeding can be increased when Toremifene is combined with Semuloparin.
Idraparinux The risk or severity of bleeding can be increased when Toremifene is combined with Idraparinux.
Cangrelor The risk or severity of bleeding can be increased when Toremifene is combined with Cangrelor.
Astaxanthin The risk or severity of bleeding can be increased when Toremifene is combined with Astaxanthin.
Apixaban The risk or severity of bleeding can be increased when Toremifene is combined with Apixaban.
Otamixaban The risk or severity of bleeding can be increased when Toremifene is combined with Otamixaban.
Amediplase The risk or severity of bleeding can be increased when Toremifene is combined with Amediplase.
Danaparoid The risk or severity of bleeding can be increased when Toremifene is combined with Danaparoid.
Dalteparin The risk or severity of bleeding can be increased when Toremifene is combined with Dalteparin.
Tinzaparin The risk or severity of bleeding can be increased when Toremifene is combined with Tinzaparin.
(R)-warfarin The risk or severity of bleeding can be increased when Toremifene is combined with (R)-warfarin.
Ethyl biscoumacetate The risk or severity of bleeding can be increased when Toremifene is combined with Ethyl biscoumacetate.
Nadroparin The risk or severity of bleeding can be increased when Toremifene is combined with Nadroparin.
Triflusal The risk or severity of bleeding can be increased when Toremifene is combined with Triflusal.
Ticagrelor The risk or severity of bleeding can be increased when Toremifene is combined with Ticagrelor.
Ditazole The risk or severity of bleeding can be increased when Toremifene is combined with Ditazole.
Vorapaxar The risk or severity of bleeding can be increased when Toremifene is combined with Vorapaxar.
Sodium citrate The risk or severity of bleeding can be increased when Toremifene is combined with Sodium citrate.
Dextran The risk or severity of bleeding can be increased when Toremifene is combined with Dextran.
Bemiparin The risk or severity of bleeding can be increased when Toremifene is combined with Bemiparin.
Parnaparin The risk or severity of bleeding can be increased when Toremifene is combined with Parnaparin.
Desirudin The risk or severity of bleeding can be increased when Toremifene is combined with Desirudin.
Antithrombin Alfa The risk or severity of bleeding can be increased when Toremifene is combined with Antithrombin Alfa.
Protein C The risk or severity of bleeding can be increased when Toremifene is combined with Protein C.
Antithrombin III human The risk or severity of bleeding can be increased when Toremifene is combined with Antithrombin III human.
Letaxaban The risk or severity of bleeding can be increased when Toremifene is combined with Letaxaban.
Darexaban The risk or severity of bleeding can be increased when Toremifene is combined with Darexaban.
Nafamostat The risk or severity of bleeding can be increased when Toremifene is combined with Nafamostat.
Monteplase The risk or severity of bleeding can be increased when Toremifene is combined with Monteplase.
Gabexate The risk or severity of bleeding can be increased when Toremifene is combined with Gabexate.
Fluindione The risk or severity of bleeding can be increased when Toremifene is combined with Fluindione.
Protein S human The risk or severity of bleeding can be increased when Toremifene is combined with Protein S human.
Brinase The risk or severity of bleeding can be increased when Toremifene is combined with Brinase.
Clorindione The risk or severity of bleeding can be increased when Toremifene is combined with Clorindione.
Diphenadione The risk or severity of bleeding can be increased when Toremifene is combined with Diphenadione.
Tioclomarol The risk or severity of bleeding can be increased when Toremifene is combined with Tioclomarol.
Melagatran The risk or severity of bleeding can be increased when Toremifene is combined with Melagatran.

Target Protein

Estrogen receptor ESR1
Sex hormone-binding globulin SHBG

Referensi & Sumber

Synthesis reference: Reijo Toivola, Tuomas Huuhtanen, "Toremifene crystallization method." U.S. Patent US20070093556, issued April 26, 2007.
Artikel (PubMed)
  • PMID: 15882476
    Price N, Sartor O, Hutson T, Mariani S: Role of 5a-reductase inhibitors and selective estrogen receptor modulators as potential chemopreventive agents for prostate cancer. Clin Prostate Cancer. 2005 Mar;3(4):211-4.
  • PMID: 16503765
    Taneja SS, Smith MR, Dalton JT, Raghow S, Barnette G, Steiner M, Veverka KA: Toremifene--a promising therapy for the prevention of prostate cancer and complications of androgen deprivation therapy. Expert Opin Investig Drugs. 2006 Mar;15(3):293-305.
  • PMID: 17644117
    Thompson IM: Chemoprevention of prostate cancer: agents and study designs. J Urol. 2007 Sep;178(3 Pt 2):S9-S13. Epub 2007 Jul 20.
  • PMID: 16515478
    Ariazi EA, Ariazi JL, Cordera F, Jordan VC: Estrogen receptors as therapeutic targets in breast cancer. Curr Top Med Chem. 2006;6(3):181-202.
  • PMID: 17504144
    Musa MA, Khan MO, Cooperwood JS: Medicinal chemistry and emerging strategies applied to the development of selective estrogen receptor modulators (SERMs). Curr Med Chem. 2007;14(11):1249-61.
  • PMID: 31643660
    Authors unspecified: Toremifene. .
  • PMID: 23062036
    Maximov PY, Lee TM, Jordan VC: The discovery and development of selective estrogen receptor modulators (SERMs) for clinical practice. Curr Clin Pharmacol. 2013 May;8(2):135-55. doi: 10.2174/1574884711308020006.

Contoh Produk & Brand

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  • Toremifene Citrate
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International Brands
  • Acapodene

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